diacetylmorphine (diamorphine, heroin)

^[1]^[2]^[3]^[4]

Epidemiology

2-fold increase in heroin overdoses 2010-2012^[2]
nonmedical use of prescription opioids is a risk factor for heroin use^[4] Pharmacokinectics:
heroin (diacetylmorphine) is rapidly hydrolyzed to 6-monoacetyl morphine, which, in turn, is hydrolyzed to morphine
both heroin & 6-monoacetyl morphine are more lipid soluble than morphine & more readily cross the blood brain barrier
intravenous injection of heroin gives a "rush" due to the rapid initial flux of heroin into the brain
this "rush" is described as a warmth, taste or high with intense pleasure & may be responsible for much of the popularity of heroin & its abuse potential
after intravenous injection, effects begin in < 1 minute
an intense euphoria "rush" ensues lasting 45 seconds to several minutes
after this, there is a period of sedation & tranquility lasting up to 1 hour
the effects of heroin wear off after 3-5 hours depending upon the dose

White house announced coordinated effort between public health & law enforcement officials to reduce heroin & prescription opioid use in certain areas of the U.S.^[3]
- goal is to shift the focus toward treatment, rather than punishment of drug users
- large-scale heroin suppliers will be targeted for arrest^[3]

↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996 pg 536, 567
↑ ^2.0 ^2.1 ^2.2 Rudd RA et al Increases in Heroin Overdose Deaths- 2010-2012. Weekly. October 3, 2014 / 63(39);849-854 http://www.cdc.gov/mmwr/preview/mmwrhtml/mm6339a1.htm
↑ ^3.0 ^3.1 ^3.2 The White House. Press Release. Aug. 17, 2015 White House Drug Policy Office Funds New Projects in High Intensity Drug Trafficking Areas. https://www.whitehouse.gov/the-press-office/2015/08/17/white-house-drug-policy-office-funds-new-projects-high-intensity-drug
↑ ^4.0 ^4.1 Compton WM, Jones CM, Baldwin GT Relationship between Nonmedical Prescription-Opioid Use and Heroin Use. N Engl J Med 2016; 374:154-163. January 14, 2016 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/26760086 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMra1508490